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AAI101 Sale

(Synonyms: Enmetazobactam) 目录号 : GC32165

A β-lactamase inhibitor

AAI101 Chemical Structure

Cas No.:1001404-83-6

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥790.00
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5mg
¥720.00
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10mg
¥1,170.00
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50mg
¥3,240.00
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100mg
¥4,860.00
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Sample solution is provided at 25 µL, 10mM.

Description

Enmetazobactam is a β-lactamase inhibitor.1 It has greater activity against class A β-lactamases (IC50s = 0.006-0.52 ?M) than class B or class D β-lactamases (IC50s = 8.7->100 ?M). Enmetazobactam in combination with the cephalosporin antibiotic cefepime is active against 223 Enterobacteriaceae clinical isolates, including multidrug-resistant E. coli and K. pneumoniae isolates, with an MIC50 value of 0.125 mg/L.2 In vivo, enmetazobactam reduces mortality in mouse models of septicemia induced by E. coli, K. pneumoniae, or E. cloacae when used in combination with cefepime.1

1.Papp-Wallace, K.M., Bethel, C.R., Caillon, J., et al.Beyond piperacillin-tazobactam: Cefepime and AAI101 as a potent β-lactam-β-lactamase inhibitor combinationAntimicrob Agents Chemother.63(5)e00105-00119(2019) 2.Crandon, J.L., and Nicolau, D.P.In vitro activity of cefepime/AAI101 and comparators against cefepime non-susceptible EnterobacteriaceaePathogens4(3)620-625(2015)

实验参考方法

Animal experiment:

The 20 Enterobacteriaceae strains are used to infect groups of three mice each. At 2 h after inoculation, mice are treated with humanized regimens of cefepime or cefepime-AAI101. All doses are administered as 0.2-mL subcutaneous injections. To serve as control animals, an additional group of mice is administered normal saline at the same volume and frequency and by the same route. Thighs from all animals are harvested at 24 h after initiation of therapy. The harvesting procedure for all study mice began with euthanasia by CO2 exposure, followed by cervical dislocation. After sacrifice, thighs are removed and homogenized individually in normal saline. For determinations of the numbers of CFU, serial dilutions of thigh homogenates are spread onto Trypticase soy agar with 5% sheep blood using a spiral plater. In addition to the aforementioned treatment and control groups, another group of three infected but untreated mice is harvested at the initiation of dosing and served as a 0-h control. Efficacy, expressed as the change in bacterial density, is determined by calculation of the change in the log10 number of CFU obtained in mice after 24 h of treatment from the densities observed in the 0-h control animals.

References:

[1]. Crandon JL, et al. In Vitro Activity of Cefepime/AAI101 and Comparators against Cefepime Non-susceptible Enterobacteriaceae. Pathogens. 2015 Aug 18;4(3):620-5.
[2]. Crandon JL, et al. In vivo activities of simulated human doses of cefepime and cefepime-AAI101 against multidrug-resistant Gram-negative Enterobacteriaceae. Antimicrob Agents Chemother. 2015 May;59(5):2688-94.

化学性质

Cas No. 1001404-83-6 SDF
别名 Enmetazobactam
Canonical SMILES C[N+]1=NN(C[C@@](S([C@]2([H])C3)(=O)=O)(C)[C@H](C([O-])=O)N2C3=O)C=C1
分子式 C11H14N4O5S 分子量 314.32
溶解度 DMSO : ≥ 113.3 mg/mL (360.46 mM) 储存条件 Store at -20°C, protect from light, stored under nitrogen
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 3.1815 mL 15.9074 mL 31.8147 mL
5 mM 0.6363 mL 3.1815 mL 6.3629 mL
10 mM 0.3181 mL 1.5907 mL 3.1815 mL
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